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Open AccessArticle

Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System

1
College of Pharmacy, Pusan National University, Busan 609-735, Korea
2
College of Pharmacy, Kyungsung University, Busan 608-736, Korea
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Author to whom correspondence should be addressed.
Academic Editor: Antonella Piozzi
Int. J. Mol. Sci. 2015, 16(5), 10821-10833; https://doi.org/10.3390/ijms160510821
Received: 16 February 2015 / Revised: 7 May 2015 / Accepted: 8 May 2015 / Published: 13 May 2015
(This article belongs to the Section Materials Science)
The purpose of this study was to prepare a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system (SMEDDS) using hydrophilic additives with high oral bioavailability, and to determine if there was a correlation between the in vitro dissolution data and the in vivo pharmacokinetic parameters of this delivery system in rats. A dutasteride-loaded solid-supersaturatable SMEDDS was generated by adsorption of liquid SMEDDS onto Aerosil 200 colloidal silica using a spray drying process. The dissolution and oral absorption of dutasteride from solid SMEDDS significantly increased after the addition of hydroxypropylmethyl cellulose (HPMC) or Soluplus. Solid SMEDDS/Aerosil 200/Soluplus microparticles had higher oral bioavailability with 6.8- and 5.0-fold higher peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) values, respectively, than that of the equivalent physical mixture. A linear correlation between in vitro dissolution efficiency and in vivo pharmacokinetic parameters was demonstrated for both AUC and Cmax values. Therefore, the preparation of a solid-supersaturatable SMEDDS with HPMC or Soluplus could be a promising formulation strategy to develop novel solid dosage forms of dutasteride. View Full-Text
Keywords: self-emulsifying; bioavailability; dutasteride; cellulose; drug delivery self-emulsifying; bioavailability; dutasteride; cellulose; drug delivery
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Kim, M.-S.; Ha, E.-S.; Choo, G.-H.; Baek, I.-H. Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System. Int. J. Mol. Sci. 2015, 16, 10821-10833.

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